Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FGFR4-IN-5, a covalent FGFR4 inhibitor, demonstrates potency and selectivity with an IC50 value of 6.5 nM. Exhibiting significant in vivo anti-tumor activity, it is applicable for research in hepatocellular carcinoma [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 2,490 | 5日内发货 | ||
25 mg | ¥ 11,700 | 6-8周 | ||
50 mg | ¥ 15,300 | 6-8周 | ||
100 mg | ¥ 19,500 | 6-8周 |
产品描述 | FGFR4-IN-5, a covalent FGFR4 inhibitor, demonstrates potency and selectivity with an IC50 value of 6.5 nM. Exhibiting significant in vivo anti-tumor activity, it is applicable for research in hepatocellular carcinoma [1]. |
靶点活性 | FGFR4:6.5 nM (IC50), FGFR2:505 nM (IC50) |
体内活性 | FGFR4-IN-5 (oral gavage; 10 mg/kg; single dose) reveals a high Cmax, low clearance, the Cmax values are 423 ng/ml, 588 ng/ml, and 2820 ng/ml in mice, rat and cynamolgus monkey, respectively. And the oral bioavailability are 20, 12, and 27% in mouse, rat, and cyno, respectively[1].FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model[1].FGFR4-IN-5 (oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days) results in dose-dependent growth inhibition of resistant tumors. Tumor regression is observed at 30 and 100 mg/kg, with %δT/δC of 67% and 70%, respectively. However, treatment with sorafenib at 100 mg/kg once daily does not provide any benefit in vivo[1]. |
别名 | FGFR4-IN-5 |
分子量 | 520.37 |
分子式 | C23H23Cl2N5O5 |
CAS No. | 1628793-01-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (192.17 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9217 mL | 9.6085 mL | 19.2171 mL | 48.0427 mL |
5 mM | 0.3843 mL | 1.9217 mL | 3.8434 mL | 9.6085 mL | |
10 mM | 0.1922 mL | 0.9609 mL | 1.9217 mL | 4.8043 mL | |
20 mM | 0.0961 mL | 0.4804 mL | 0.9609 mL | 2.4021 mL | |
50 mM | 0.0384 mL | 0.1922 mL | 0.3843 mL | 0.9609 mL | |
100 mM | 0.0192 mL | 0.0961 mL | 0.1922 mL | 0.4804 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
FGFR4-IN-5 1628793-01-0 FGFR4 IN 5 FGFR-4-IN-5 FGFR4IN5 Inhibitor inhibitor inhibit